JP2005501091A5 - - Google Patents
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- Publication number
- JP2005501091A5 JP2005501091A5 JP2003519060A JP2003519060A JP2005501091A5 JP 2005501091 A5 JP2005501091 A5 JP 2005501091A5 JP 2003519060 A JP2003519060 A JP 2003519060A JP 2003519060 A JP2003519060 A JP 2003519060A JP 2005501091 A5 JP2005501091 A5 JP 2005501091A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- hydrolyzed
- vivo
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 30
- 125000000217 alkyl group Chemical group 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 26
- 239000011780 sodium chloride Substances 0.000 claims 26
- 150000002148 esters Chemical class 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 230000001404 mediated Effects 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 102000014961 Protein Precursors Human genes 0.000 claims 2
- 108010078762 Protein Precursors Proteins 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- OZAIFHULBGXAKX-UHFFFAOYSA-N precursor Substances N#CC(C)(C)N=NC(C)(C)C#N OZAIFHULBGXAKX-UHFFFAOYSA-N 0.000 claims 2
- 206010003246 Arthritis Diseases 0.000 claims 1
- 102100004962 MMP13 Human genes 0.000 claims 1
- 101700084657 MMP13 Proteins 0.000 claims 1
- 108010006035 Metalloproteases Proteins 0.000 claims 1
- 102000005741 Metalloproteases Human genes 0.000 claims 1
- MEPZIAABDIWXRB-QHELBMECSA-N N-[(4S)-1-[4-(4-ethynylphenyl)piperazin-1-yl]sulfonyl-4-phenylpentan-2-yl]-N-hydroxyformamide Chemical compound C([C@H](C)C=1C=CC=CC=1)C(N(O)C=O)CS(=O)(=O)N(CC1)CCN1C1=CC=C(C#C)C=C1 MEPZIAABDIWXRB-QHELBMECSA-N 0.000 claims 1
- RXWBWBFRSYEARG-UHFFFAOYSA-N N-[1-[4-[5-[2-(4-fluorophenyl)ethynyl]pyridin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]-N-hydroxyformamide Chemical compound C1CN(C=2N=CC(=CC=2)C#CC=2C=CC(F)=CC=2)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 RXWBWBFRSYEARG-UHFFFAOYSA-N 0.000 claims 1
- IITOQKJCTHQVBH-DEOSSOPVSA-N N-hydroxy-N-[(2S)-1-[4-[5-(2-pyridin-2-ylethynyl)pyridin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C([C@H](N(C=O)O)CS(=O)(=O)N1CCN(CC1)C=1N=CC(=CC=1)C#CC=1N=CC=CC=1)CCC1=NC=CC=N1 IITOQKJCTHQVBH-DEOSSOPVSA-N 0.000 claims 1
- MHKMIMPCEDHDDQ-QHCPKHFHSA-N N-hydroxy-N-[(2S)-1-[4-[5-(2-pyridin-2-ylethynyl)pyrimidin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C([C@H](N(C=O)O)CS(=O)(=O)N1CCN(CC1)C=1N=CC(=CN=1)C#CC=1N=CC=CC=1)CCC1=NC=CC=N1 MHKMIMPCEDHDDQ-QHCPKHFHSA-N 0.000 claims 1
- DGDVSMKFNJQMMB-SUHMBNCMSA-N N-hydroxy-N-[(4S)-4-phenyl-1-[4-[4-(2-phenylethynyl)phenyl]piperazin-1-yl]sulfonylpentan-2-yl]formamide Chemical compound C([C@H](C)C=1C=CC=CC=1)C(N(O)C=O)CS(=O)(=O)N(CC1)CCN1C(C=C1)=CC=C1C#CC1=CC=CC=C1 DGDVSMKFNJQMMB-SUHMBNCMSA-N 0.000 claims 1
- IITOQKJCTHQVBH-UHFFFAOYSA-N N-hydroxy-N-[1-[4-[5-(2-pyridin-2-ylethynyl)pyridin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C1CN(C=2N=CC(=CC=2)C#CC=2N=CC=CC=2)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 IITOQKJCTHQVBH-UHFFFAOYSA-N 0.000 claims 1
- MHKMIMPCEDHDDQ-UHFFFAOYSA-N N-hydroxy-N-[1-[4-[5-(2-pyridin-2-ylethynyl)pyrimidin-2-yl]piperazin-1-yl]sulfonyl-5-pyrimidin-2-ylpentan-2-yl]formamide Chemical compound C1CN(C=2N=CC(=CN=2)C#CC=2N=CC=CC=2)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 MHKMIMPCEDHDDQ-UHFFFAOYSA-N 0.000 claims 1
- BQBUHHIWALLHGP-UHFFFAOYSA-N N-hydroxy-N-[5-pyrimidin-2-yl-1-[4-[5-(2-thiophen-2-ylethynyl)pyridin-2-yl]piperazin-1-yl]sulfonylpentan-2-yl]formamide Chemical compound C1CN(C=2N=CC(=CC=2)C#CC=2SC=CC=2)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 BQBUHHIWALLHGP-UHFFFAOYSA-N 0.000 claims 1
- AMFADHXFVRMZAZ-UHFFFAOYSA-N N-hydroxy-N-[5-pyrimidin-2-yl-1-[4-[5-[2-[5-(trifluoromethyl)pyridin-2-yl]ethynyl]pyridin-2-yl]piperazin-1-yl]sulfonylpentan-2-yl]formamide Chemical compound C1CN(C=2N=CC(=CC=2)C#CC=2N=CC(=CC=2)C(F)(F)F)CCN1S(=O)(=O)CC(N(C=O)O)CCCC1=NC=CC=N1 AMFADHXFVRMZAZ-UHFFFAOYSA-N 0.000 claims 1
- 125000005418 aryl aryl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0119474.5A GB0119474D0 (en) | 2001-08-09 | 2001-08-09 | Compounds |
| PCT/SE2002/001436 WO2003014111A1 (en) | 2001-08-09 | 2002-08-08 | Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005501091A JP2005501091A (ja) | 2005-01-13 |
| JP2005501091A5 true JP2005501091A5 (da) | 2006-01-12 |
Family
ID=9920126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003519060A Pending JP2005501091A (ja) | 2001-08-09 | 2002-08-08 | アリールピペラジンとアリールピペリジン、およびメタロプロテイナーゼ阻害剤としてのそれらの使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US7153857B2 (da) |
| EP (1) | EP1417201A1 (da) |
| JP (1) | JP2005501091A (da) |
| GB (1) | GB0119474D0 (da) |
| WO (1) | WO2003014111A1 (da) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7452911B2 (en) | 2002-10-31 | 2008-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| DE10250708A1 (de) * | 2002-10-31 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7351719B2 (en) | 2002-10-31 | 2008-04-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds |
| US7592373B2 (en) | 2003-12-23 | 2009-09-22 | Boehringer Ingelheim International Gmbh | Amide compounds with MCH antagonistic activity and medicaments comprising these compounds |
| US7524862B2 (en) | 2004-04-14 | 2009-04-28 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| DE102004017930A1 (de) * | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US20050245529A1 (en) * | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim International Gmbh | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| DE102004017934A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7776869B2 (en) | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| EP2923703B1 (en) | 2006-12-15 | 2018-09-19 | NantBio, Inc. | Triazine derivatives and their therapeutical applications |
| WO2010144394A1 (en) | 2009-06-09 | 2010-12-16 | Abraxis Bioscience, Llc | Benzyl substituted triazine derivatives and their therapeutical applications |
| WO2010144550A1 (en) | 2009-06-09 | 2010-12-16 | Abraxis Bioscience, Llc | Triazine derivatives and their therapeutical applications |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH27291A (en) | 1989-01-31 | 1993-05-04 | Takeda Chemical Industries Ltd | Imidazolpyrimidazines their production and use |
| US5552419A (en) * | 1993-01-06 | 1996-09-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5506242A (en) | 1993-01-06 | 1996-04-09 | Ciba-Geigy Corporation | Arylsufonamido-substituted hydroxamic acids |
| US5646167A (en) | 1993-01-06 | 1997-07-08 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamix acids |
| US5817822A (en) * | 1994-06-24 | 1998-10-06 | Novartis Corporation | Certain alpha-azacycloalkyl substituted arylsulfonamido acetohydroxamic acids |
| CA2263154A1 (en) | 1996-08-07 | 1998-02-12 | Darwin Discovery Limited | Hydroxamic and carboxylic acid derivatives having mmp and tnf inhibitory activity |
| AU743901B2 (en) | 1996-10-16 | 2002-02-07 | Wyeth Holdings Corporation | Ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloprote inase and tace inhibitors |
| ZA98376B (en) * | 1997-01-23 | 1998-07-23 | Hoffmann La Roche | Sulfamide-metalloprotease inhibitors |
| US6376506B1 (en) * | 1997-01-23 | 2002-04-23 | Syntex (U.S.A.) Llc | Sulfamide-metalloprotease inhibitors |
| TR199901765T2 (xx) | 1997-01-23 | 1999-10-21 | F.Hoffmann-La Roche Ag | S�lfomid-metalloproteaz inhibit�rleri |
| CA2265671A1 (en) | 1997-07-10 | 1999-01-21 | Daniela Jabes | Matrix metalloproteinase inhibitors |
| US6482827B1 (en) * | 1997-07-10 | 2002-11-19 | Pharmacia & Upjohn S.P.A. | Matrix metalloproteinase inhibitors |
| US6235786B1 (en) * | 1997-08-06 | 2001-05-22 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| US6294573B1 (en) * | 1997-08-06 | 2001-09-25 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| US6403632B1 (en) * | 2000-03-01 | 2002-06-11 | Bristol Myers Squibb Pharma Co | Lactam metalloprotease inhibitors |
| ZA988967B (en) | 1997-10-03 | 2000-04-03 | Du Pont Pharm Co | Lactam metalloprotease inhibitors. |
| US6130220A (en) * | 1997-10-16 | 2000-10-10 | Syntex (Usa) Inc. | Sulfamide-metalloprotease inhibitors |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| PL200418B1 (pl) | 1998-01-30 | 2009-01-30 | Darwin Discovery Ltd | Pochodna N-hydroksyformamidu, zawierający ją środek farmaceutyczny i jej zastosowanie |
| EP1107953A1 (en) | 1998-08-29 | 2001-06-20 | British Biotech Pharmaceuticals Limited | Hydroxamic acid derivatives as proteinase inhibitors |
| GB9919776D0 (en) * | 1998-08-31 | 1999-10-27 | Zeneca Ltd | Compoujnds |
| GEP20043238B (en) * | 1999-02-08 | 2004-05-25 | Searle & Co | Sulfamato Hydroxamic Acid Metalloprotease Inhibitor, its Use in Preparation of Pharmaceutical Composition for Treatment of Conditions Associated with Pathological Matrix Metalloprotease Activity |
| US6511993B1 (en) * | 1999-06-03 | 2003-01-28 | Kevin Neil Dack | Metalloprotease inhibitors |
| NZ515829A (en) | 1999-06-04 | 2003-10-31 | Astrazeneca Ab | Inhibitors of metalloproteinases |
| EP1261595A1 (en) * | 2000-02-21 | 2002-12-04 | AstraZeneca AB | Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents |
| HUP0302723A3 (en) | 2000-02-21 | 2007-09-28 | Astrazeneca Ab | Piperidine- and piperazine substituted n-hydroxyformamides as inhibitors of metalloproteinases, process for their preparation and pharmaceutical compositions containing them |
| JP2003524007A (ja) | 2000-02-21 | 2003-08-12 | アストラゼネカ・アクチエボラーグ | アリールピペラジン類およびそれらのメタロプロテイナーゼ阻害剤（ｍｍｐ）としての使用 |
| CA2409035A1 (en) * | 2000-05-15 | 2001-11-22 | Darwin Discovery Limited | Hydroxamic acid derivatives |
| GB0119473D0 (en) | 2001-08-09 | 2001-10-03 | Astrazeneca | Compounds |
| GB0119472D0 (en) | 2001-08-09 | 2001-10-03 | Astrazeneca Ab | Compounds |
-
2001
- 2001-08-09 GB GBGB0119474.5A patent/GB0119474D0/en not_active Ceased
-
2002
- 2002-08-08 EP EP02759021A patent/EP1417201A1/en not_active Withdrawn
- 2002-08-08 JP JP2003519060A patent/JP2005501091A/ja active Pending
- 2002-08-08 WO PCT/SE2002/001436 patent/WO2003014111A1/en active Application Filing
- 2002-08-08 US US10/485,409 patent/US7153857B2/en not_active Expired - Fee Related
-
2006
- 2006-06-12 US US11/451,683 patent/US20060229313A1/en not_active Abandoned
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